A-α-CAO induces weak analgesia with very short duration in mice and is able to antagonize the analgesic effect of morphine (Mor) up to 3—4 days after a single injection. No tendency of dependence has been observed. ...A-α-CAO induces weak analgesia with very short duration in mice and is able to antagonize the analgesic effect of morphine (Mor) up to 3—4 days after a single injection. No tendency of dependence has been observed. It acts as a partial agonist on MVD with Ke value of 9×10^(-9) mol/L. Its antagonist effect remains after several washes and its agonist effect cannot be reversed by naloxone (Nx), provided the incubation time or the concentration of the agent is sufficient. On isolated GPI, A-α-CAO is a pure agonist with IC_(50) of 5.7×10^(-10) mol/L; this agonist effect cannot be removed by washing but can be reversed by Nx. On RVD and RbVD, it has antagonist effect against β-endorphine (β-end) and US0488H, which cannot be washed out easily, and the pA_2are 7.5 and 7.6 respectively. A-α-CAO also inhibits the specific binding of ~3H-etorphine (~3H-Etor) to the P_2 fraction of the mouse brain membrane with an IC_(30) of 3.2×10^(-9) mol/L. The inhibition on the high affinity binding sites of ~3H-Etor remains 95％ even after 6 washes.展开更多
目的考察手术期间不同时间点给予地佐辛辅助镇痛对妇科手术患者全身麻醉苏醒质量的影响。方法择期妇科手术患者90例，美国麻醉医师协会（ASA）分级I～Ⅱ级，采用随机数字表法分为3组：A组，手术开始前10min静脉注射地佐辛0．1mg／kg；B...目的考察手术期间不同时间点给予地佐辛辅助镇痛对妇科手术患者全身麻醉苏醒质量的影响。方法择期妇科手术患者90例，美国麻醉医师协会（ASA）分级I～Ⅱ级，采用随机数字表法分为3组：A组，手术开始前10min静脉注射地佐辛0．1mg／kg；B组，手术结束前30min静脉注射地佐辛0．1mg／kg；C组，对照组，在同等时间静脉注射等量生理盐水。麻醉诱导：咪达唑仑0．05mg／kg，依托咪酯0．3mg／kg，舒芬太尼0．5μg／kg，维库溴铵闭环输注0．1mg／kg诱导。采用统一标准的精确化麻醉管理，丙泊酚靶控输注2．0mg／L～2．5mg／L，脑电双频指数（bispectral index，BIS）监测维持在40—50，气体浓度监测七氟醚0．3最低肺泡有效浓度（minimalal veolar concentration，MAC）～0．5MAC吸入，维库溴铵闭环输注维持肌松（增药条件：T1〉7％），舒芬太尼持续泵注0．2μg·kg^-1·h^-1（术前0．5h停药），手术结束，BIS〉60，T1〉90％，送麻醉后监测治疗室（post-anesthesia care unit，PACU），观察PACU期间苏醒质量[PACU驻留时间、拔管时间、清醒时间、视觉模拟评分（visual analog scale，VAS）、有无相关并发症]。术后1、2、6、24h随访，记录患者疼痛VAS评分，观察有无恶心、呕吐等阿片类药物相关副作用及患者总体满意度。结果3组患者年龄、体重指数、手术时间、麻醉时间、拔管时间、PACU驻留时间、丙泊酚用量差异均无统计学意义。3组患者清醒时间比较：A组（12±2）min，B组（8±1）min，C组（13±3）min，B组较A组、C组苏醒迅速（P〈0．05），A组、C组间比较差异无统计学意义。拔管后呼吸抑制的发生率比较：A组3／30（10％），B组0／30（0），C组0／30（0），A组较B组、c组呼吸抑制发生明显增多（P〈0．05），B组、C组间比较差异无统计学意义。术后2hVAS评分：A组（0．50±0．73）分，B组（0．33±0．48展开更多
基金This work was partly supported by the National Natural Science Foundation of China. A part of the data has been presented on a China-US Neuroscience Conference sponsored by Academia Sinica and National Academy of Science, USA, June 7-11, 1986, at Shangh
文摘A-α-CAO induces weak analgesia with very short duration in mice and is able to antagonize the analgesic effect of morphine (Mor) up to 3—4 days after a single injection. No tendency of dependence has been observed. It acts as a partial agonist on MVD with Ke value of 9×10^(-9) mol/L. Its antagonist effect remains after several washes and its agonist effect cannot be reversed by naloxone (Nx), provided the incubation time or the concentration of the agent is sufficient. On isolated GPI, A-α-CAO is a pure agonist with IC_(50) of 5.7×10^(-10) mol/L; this agonist effect cannot be removed by washing but can be reversed by Nx. On RVD and RbVD, it has antagonist effect against β-endorphine (β-end) and US0488H, which cannot be washed out easily, and the pA_2are 7.5 and 7.6 respectively. A-α-CAO also inhibits the specific binding of ~3H-etorphine (~3H-Etor) to the P_2 fraction of the mouse brain membrane with an IC_(30) of 3.2×10^(-9) mol/L. The inhibition on the high affinity binding sites of ~3H-Etor remains 95％ even after 6 washes.
文摘目的考察手术期间不同时间点给予地佐辛辅助镇痛对妇科手术患者全身麻醉苏醒质量的影响。方法择期妇科手术患者90例，美国麻醉医师协会（ASA）分级I～Ⅱ级，采用随机数字表法分为3组：A组，手术开始前10min静脉注射地佐辛0．1mg／kg；B组，手术结束前30min静脉注射地佐辛0．1mg／kg；C组，对照组，在同等时间静脉注射等量生理盐水。麻醉诱导：咪达唑仑0．05mg／kg，依托咪酯0．3mg／kg，舒芬太尼0．5μg／kg，维库溴铵闭环输注0．1mg／kg诱导。采用统一标准的精确化麻醉管理，丙泊酚靶控输注2．0mg／L～2．5mg／L，脑电双频指数（bispectral index，BIS）监测维持在40—50，气体浓度监测七氟醚0．3最低肺泡有效浓度（minimalal veolar concentration，MAC）～0．5MAC吸入，维库溴铵闭环输注维持肌松（增药条件：T1〉7％），舒芬太尼持续泵注0．2μg·kg^-1·h^-1（术前0．5h停药），手术结束，BIS〉60，T1〉90％，送麻醉后监测治疗室（post-anesthesia care unit，PACU），观察PACU期间苏醒质量[PACU驻留时间、拔管时间、清醒时间、视觉模拟评分（visual analog scale，VAS）、有无相关并发症]。术后1、2、6、24h随访，记录患者疼痛VAS评分，观察有无恶心、呕吐等阿片类药物相关副作用及患者总体满意度。结果3组患者年龄、体重指数、手术时间、麻醉时间、拔管时间、PACU驻留时间、丙泊酚用量差异均无统计学意义。3组患者清醒时间比较：A组（12±2）min，B组（8±1）min，C组（13±3）min，B组较A组、C组苏醒迅速（P〈0．05），A组、C组间比较差异无统计学意义。拔管后呼吸抑制的发生率比较：A组3／30（10％），B组0／30（0），C组0／30（0），A组较B组、c组呼吸抑制发生明显增多（P〈0．05），B组、C组间比较差异无统计学意义。术后2hVAS评分：A组（0．50±0．73）分，B组（0．33±0．48
